Page last updated: 2024-08-07 16:43:38
Melatonin receptor type 1A
A melatonin receptor type 1A that is encoded in the genome of human. [PRO:WCB, UniProtKB:P48039]
Synonyms
Mel-1A-R;
Mel1a receptor
Research
Bioassay Publications (77)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 9 (11.69) | 18.2507 |
| 2000's | 30 (38.96) | 29.6817 |
| 2010's | 30 (38.96) | 24.3611 |
| 2020's | 8 (10.39) | 2.80 |
Compounds (28)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| umbelliprenin | Homo sapiens (human) | KiH | 0.0016 | 1 | 1 |
| umbelliprenin | Homo sapiens (human) | KiL | 0.0033 | 1 | 1 |
Design and Validation of the First Family of Photo-Activatable Ligands for Melatonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
[no title available]Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
[no title available]Journal of medicinal chemistry, , 02-25, Volume: 64, Issue:4, 2021
Tuning melatonin receptor subtype selectivity in oxadiazolone-based analogues: Discovery of QR2 ligands and NRF2 activators with neurogenic properties.European journal of medicinal chemistry, , Mar-15, Volume: 190, 2020
Indole-based melatonin analogues: Synthetic approaches and biological activity.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Polybenzyls from Gastrodia elata, their agonistic effects on melatonin receptors and structure-activity relationships.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
[no title available]Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Oxyprenylated Phenylpropanoids Bind to MT1 Melatonin Receptors and Inhibit Breast Cancer Cell Proliferation and Migration.Journal of natural products, , 12-22, Volume: 80, Issue:12, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Synthesis of 2-arylfuro[3,2-b]pyridines: Effect of the C2-aryl group on melatoninergic activity.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
New coumarin-based fluorescent melatonin ligands. Design, synthesis and pharmacological characterization.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
Synthesis of new melatoninergic hexahydroindenopyridines.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Efficient synthesis of hexahydroindenopyridines and their potential as melatoninergic ligands.European journal of medicinal chemistry, , Oct-30, Volume: 86, 2014
Development of substituted N-[3-(3-methoxylphenyl)propyl] amides as MT(2)-selective melatonin agonists: improving metabolic stability.Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Synthesis of new N-(arylcyclopropyl)acetamides and N-(arylvinyl)acetamides as conformationally-restricted ligands for melatonin receptors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 23, Issue:2, 2013
Design and synthesis of 2-phenylimidazo[1,2-a]pyridines as a novel class of melatonin receptor ligands.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Preparation and pharmacological evaluation of a novel series of 2-(phenylthio)benzo[b]thiophenes as selective MT2 receptor ligands.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011
Synthesis of a novel series of tricyclic dihydrofuran derivatives: discovery of 8,9-dihydrofuro[3,2-c]pyrazolo[1,5-a]pyridines as melatonin receptor (MT1/MT2) ligands.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
1,6-Dihydro-2H-indeno[5,4-b]furan derivatives: design, synthesis, and pharmacological characterization of a novel class of highly potent MTâ‚‚-selective agonists.Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Design and synthesis of 1-(2-alkanamidoethyl)-6-methoxy-7-azaindole derivatives as potent melatonin agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
Design and synthesis of naphthalenic derivatives as new ligands at the melatonin binding site MT3.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011
Bivalent ligand approach on N-{2-[(3-methoxyphenyl)methylamino]ethyl}acetamide: synthesis, binding affinity and intrinsic activity for MT(1) and MT(2) melatonin receptors.Bioorganic & medicinal chemistry, , Aug-15, Volume: 19, Issue:16, 2011
Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands.Bioorganic & medicinal chemistry, , May-15, Volume: 18, Issue:10, 2010
Design, synthesis, and pharmacological effects of structurally simple ligands for MT(1) and MT(2) melatonin receptors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 18, Issue:17, 2010
Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Synthesis and pharmacological evaluation of 1,2,3,4-tetrahydropyrazino[1,2-a]indole and 2-[(phenylmethylamino)methyl]-1H-indole analogues as novel melatoninergic ligands.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Synthesis of 3-phenylnaphthalenic derivatives as new selective MT(2) melatoninergic ligands.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3.Bioorganic & medicinal chemistry, , May-01, Volume: 16, Issue:9, 2008
Synthesis and pharmacological evaluation of pentacyclic 6a,7-dihydrodiindole and 2,3-dihydrodiindole derivatives as novel melatoninergic ligands.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
7-Substituted-melatonin and 7-substituted-1-methylmelatonin analogues: effect of substituents on potency and binding affinity.Bioorganic & medicinal chemistry, , Jul-01, Volume: 15, Issue:13, 2007
Design, synthesis and melatoninergic activity of new unsubstituted and beta,beta'-difunctionalised 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-alkanamides.European journal of medicinal chemistry, , Volume: 42, Issue:7, 2007
Synthesis and biological activity of new melatonin dimeric derivatives.Bioorganic & medicinal chemistry, , Jul-01, Volume: 15, Issue:13, 2007
N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Design and synthesis of N-(3,3-diphenylpropenyl)alkanamides as a novel class of high-affinity MT2-selective melatonin receptor ligands.Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-methoxy-1-methyltryptamines.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
Design and synthesis of benzoxazole derivatives as novel melatoninergic ligands.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 14, Issue:5, 2004
Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.Bioorganic & medicinal chemistry letters, , Jul-16, Volume: 14, Issue:14, 2004
Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
4-Substituted anilides as selective melatonin MT2 receptor agonists.Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Indanyl piperazines as melatonergic MT2 selective agents.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands.Journal of medicinal chemistry, , Mar-27, Volume: 46, Issue:7, 2003
Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Synthesis of a novel series of benzocycloalkene derivatives as melatonin receptor agonists.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Synthesis and structure-affinity-activity relationships of novel benzofuran derivatives as MT(2) melatonin receptor selective ligands.Journal of medicinal chemistry, , Jun-20, Volume: 45, Issue:13, 2002
Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3).Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
2-N-acylaminoalkylindoles: design and quantitative structure-activity relationship studies leading to MT2-selective melatonin antagonists.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Synthesis of phenalene and acenaphthene derivatives as new conformationally restricted ligands for melatonin receptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Pharmacophoric search and 3D-QSAR comparative molecular field analysis studies on agonists of melatonin sheep receptors.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
Melatonin receptor ligands: synthesis of new melatonin derivatives and comprehensive comparative molecular field analysis (CoMFA) study.Journal of medicinal chemistry, , Sep-24, Volume: 41, Issue:20, 1998
2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
Development of a high-affinity ligand that binds irreversibly to Mel1b melatonin receptors.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
Synthesis and structure-activity relationships of novel naphthalenic and bioisosteric related amidic derivatives as melatonin receptor ligands.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
Indole-based melatonin analogues: Synthetic approaches and biological activity.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities.RSC medicinal chemistry, , Oct-19, Volume: 13, Issue:10, 2022
Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Synthesis of new N-(arylcyclopropyl)acetamides and N-(arylvinyl)acetamides as conformationally-restricted ligands for melatonin receptors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 23, Issue:2, 2013
Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands.Bioorganic & medicinal chemistry, , May-15, Volume: 18, Issue:10, 2010
Synthesis of 3-phenylnaphthalenic derivatives as new selective MT(2) melatoninergic ligands.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands.Journal of medicinal chemistry, , Mar-27, Volume: 46, Issue:7, 2003
Synthesis of phenalene and acenaphthene derivatives as new conformationally restricted ligands for melatonin receptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Synthesis and structure-activity relationships of novel naphthalenic and bioisosteric related amidic derivatives as melatonin receptor ligands.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3).Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Pharmacophoric search and 3D-QSAR comparative molecular field analysis studies on agonists of melatonin sheep receptors.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Design, synthesis and melatoninergic activity of new unsubstituted and beta,beta'-difunctionalised 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-alkanamides.European journal of medicinal chemistry, , Volume: 42, Issue:7, 2007
Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
Indole-based melatonin analogues: Synthetic approaches and biological activity.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
[no title available]Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities.RSC medicinal chemistry, , Oct-19, Volume: 13, Issue:10, 2022
1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
2-N-acylaminoalkylindoles: design and quantitative structure-activity relationship studies leading to MT2-selective melatonin antagonists.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| melatonin receptor activity | molecular function | Combining with melatonin, N-acetyl-5-methoxytryptamine, to initiate a change in cell activity. Melatonin is a neuroendocrine substance that stimulates the aggregation of melanosomes in melanophores, thus lightening the skin. [GOC:ai, ISBN:0198506732] |
| hormone binding | molecular function | Binding to an hormone, a naturally occurring substance secreted by specialized cells that affect the metabolism or behavior of cells possessing functional receptors for the hormone. Hormones may be produced by the same, or different, cell as express the receptor. [GOC:jl] |
| organic cyclic compound binding | molecular function | Binding to an organic cyclic compound, any molecular entity that contains carbon arranged in a cyclic molecular structure. [GOC:sjw, PMID:7583672] |
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| mating behavior | biological process | The behavioral interactions between organisms for the purpose of mating, or sexual reproduction resulting in the formation of zygotes. [GOC:ai, GOC:dph] |
| circadian rhythm | biological process | Any biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:bf, GOC:go_curators] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |